Synthesis and bovine beta-3 adrenergic agonistic activities of a novel series of aryloxypropanolamines.

We synthesized a novel series of 21 aryloxypropanolamine compounds characterized by N-alkyl, aralkyl, and aryl substituents. The compounds showed potent β 3 -adrenergic agonistic activities in Chinese hamster ovary cells expressing the bovine β 3 -adrenoceptors with K act and K i values of 4.2 ± 3.0 nM and 459 ± 169 nM respectively, for the ligand with the best compromise between potency and affinity. Structure-activity relationships are discussed.